CAS: 555-57-7; N-Benzyl-N-Methylprop-2-Yn-1-Amine

该化合物是一种主要用于治疗高血压和抗抑郁剂的单胺氧化酶抑制剂(MAOI),被归类为有机化合物,其特点是能够抑制单胺氧化酶酶的活动,这种酶酶在诸如血清素,无肾上腺素和多巴胺等...

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CAS号106-96-7 溴代丙炔 | CAS号103-67-3 N-甲基苄胺 | CAS号35161-71-8 N-甲基炔丙基胺 | CAS号100-52-7 苯甲醛 | CAS号111831-90-4 N-Benzyl-2-brom... | CAS号62505-91-3 5-[benzyl(methy... | CAS号622-29-7 N-苄烯甲胺 | CAS号1197-51-9 N-苄基丙-2-炔-1-胺 | CAS号100-52-7 苯甲醛

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    📜5-[苄基(甲基)氨基]-2-甲基戊-3-炔-2-醇 反应生成 优降宁
    参考文献:2-甲基-3-丁炔-2-醇在曼尼希反应中作为乙炔前体.单胺氧化酶自杀灭活剂的新合成.
    标题:2-甲基-3-丁炔-2-醇在曼尼希反应中作为乙炔前体.单胺氧化酶自杀灭活剂的新合成.
    摘要:
    DOI:10.1021/jo00435A026

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-2004053355-A1
    优先权日:2000-05-26
    标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors
    发明人:WAINER IRVING; MARKOGLOU NEKTARIA
    摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.

    专利号:US-7109377-B2
    优先权日:1996-10-16
    标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
    发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R
    权利人:HARVARD COLLEGE
    摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

    专利号:US-6362009-B1
    优先权日:1997-11-21
    标 题 :Solid phase synthesis of heterocycles
    发明人:MUNOZ BENITO; CHEN CHIXU
    权利人:MERCK & CO INC
    摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

    专利号:US-8278296-B2
    优先权日:2006-08-10
    标题:Manipulation of brain CDP-diacylglycerol and uses thereof
    发明人:UNDIEH ASHIWEL S
    权利人:UNDIEH ASHIWEL S
    摘要:Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.

    专利号:US-4310535-A
    优先权日:1976-11-30
    标题:Combination of drugs and a method for the selective control of the immune reactions evoked in a host by the administration of antigens
    发明人:PIERPAOLI WALTER
    权利人:PIERPAOLI WALTER
    摘要:The invention concerns a new composition or combination of drugs effective to selectively control the immune reactions which are evoked in a host by the administration of antigens. It comprises active components capable of simultaneously blocking the alpha -adrenergic receptors of the cells for catecholamine, blocking the dopaminergic receptors of the cells and increasing the synthesis of serotonin. Preferred drug combinations according to the invention contain in association phentolamine, haloperidol, L-5-hydroxy-tryptophane and possibly dopamine.

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    主要参考文献


    1: Bazzu G, Rocchitta G, Migheli R, Alvau MD, Zinellu M, Puggioni G, Calia G, Mercanti G, Giusti P, Desole MS, Serra PA. Effects of the neurotoxin MPTP and pargyline protection on extracellular energy metabolites and dopamine levels in the striatum of freely moving rats. Brain Res. 2013 Nov 13;1538:159-71. doi: 10.1016/j.brainres.2013.09.037. Epub 2013 Sep 27. doi: 10.1021/acs.orglett.5b00730. Epub 2015 Apr 23. doi: 10.1021/bi101722b. Epub 2011 Mar 7.
    4: Rao BV, Manmode S, Hotha S. Propargyl 1,2-orthoesters for a catalytic and stereoselective synthesis of pyrimidine nucleosides. J Org Chem. 2015 Feb 6;80(3):1499-505. doi: 10.1021/jo502413z. Epub 2015 Jan 8.

    合成参考文献


    摘要:Anderson, E. A.; Lim, D. S. W., Science of Synthesis Knowledge Updates, (2015) 1, 144.
    摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#02420
    摘要:Toxicology of Drugs and Chemicals, Deichmann, W.B., New York, Academic Press, Inc., 1969, -(452), 1969
    摘要:Therapie., 22(367), 1967 []
    摘要:Biochemical Pharmacology., 17(369), 1968 []
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